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39

抑制剂 & 化合物

3

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Cat. No. Product Name Target Signaling Pathways
TP2315 glatiramer Acetate

Others Others
Glatiramer acetate 是髓鞘碱性蛋白的合成类似物和免疫调节剂,可用于多发性硬化症的研究。它能够诱导 T 辅助细胞 2 的特异性抑制细胞迁移到大脑并导致原位旁观者抑制。它能够于 MHC 分子强而杂乱的结合,因此与各种髓鞘抗原竞争,使其呈现给 T 细胞。
T28169 NIBR-0213

NIBR 0213

LPL Receptor GPCR/G Protein
NIBR-0213 是S1P1选择性拮抗剂,有抗实验性自身免疫性脑脊髓炎的作用。在 GTPγ35S 试验中,它作用于人和大鼠S1P1的IC50分别为 2.0 nM 和 2.3 nM。
T24984 5J-4

Calcium Channel Membrane transporter/Ion channel; Metabolism
5J-4 是一种有效的钙释放激活钙通道 (CRAC) 和钙池操纵性钙内流(SOCE) 阻滞剂。 5J-4 减少 IL-17 的产生并降低 RORα 和 RORγt 的表达。
T15795 Luzindole

N-乙酰-2-苄基色胺,N-0774

Melatonin Receptor; MT Receptor GPCR/G Protein; Neuroscience
Luzindole (N-0774) 是一种选择性褪黑素受体拮抗剂,可抑制实验性自身免疫性脑脊髓炎,有抗抑郁样活性。它优先靶向 MT2 (Mel1b),对于人 MT2 和 MT1 的 Ki 值分别为 10.2 和 158 nM。
T0994 Ketotifen fumarate

HC 20511 fumarate,富马酸酮替芬

PDE; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience
Ketotifen fumarate (HC 20511 fumarate) 是组胺 H1 受体和炎症介质释放的环七噻吩阻滞剂。
T14924 Cenerimod

ACT-334441

S1P Receptor GPCR/G Protein
Cenerimod (ACT-334441) 是一种具有口服活性、选择性和高效性的磷酸鞘氨醇 1 受体(S1P1)激动剂(EC50:1 nM)。Cenerimod 对多种 S1P 的亚型具有抑制作用,可用于研究鼠类实验性自身免疫性脑脊髓炎 (EAE)和鼠类硬皮病。
T24398 Lenaldekar

LDK

Akt; IGF-1R; S6 Kinase Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
Lenaldekar (LDK) 抑制 T 细胞扩增和自身免疫性脑脊髓炎。 Lenaldekar 导致 PI3 激酶/AKT/mTOR 通路成员的去磷酸化并延迟有丝分裂晚期的敏感细胞。
T19107 24, 25-Dihydroxy VD2

24,25-Dihydroxy vitamin D2

Vitamin Metabolism
24, 25-Dihydroxy VD2 (24,25-Dihydroxy vitamin D2) 是维生素 D2 的 代谢产物,是维生素 D在体内存在25 羟维生素 D 的异构体。
T12422 PF-04957325

PDE Metabolism
PF-04957325 是 PDE8 的抑制剂,具有高效性和选择性。PF-04957325 对 PDE8A的IC50为 0.7 nM ,对 PDE8B 的 IC50 为 0.3 nM。PF-04957325 可用于研究自身免疫性脑脊髓炎。
T77555 3-Methoxycatechol

1,2-Dihydroxy-3-methoxybenzene

Antiviral Immunology/Inflammation
3-Methoxycatechol 是一种木质素衍生的可再生化学品,可促进食管发生癌变。1,2-Dihydroxy-3-methoxybenzen 对脑脊髓炎病毒(EMCV)表现出很强的抗病毒活性.
T10385 ASP-4058

S1P Receptor; LPL Receptor GPCR/G Protein
ASP-4058 是一种鞘氨醇磷酸受体 1 和 5 (S1P1 and S1P5) 的二代激动剂,具有选择性、安全性和口服活性。ASP-4058能改善小鼠实验性自身免疫性脑脊髓炎。
T3701 MCC950

CP-456773

NOD Immunology/Inflammation; NF-κB
MCC950 (CP-456773) 是NLRP3的选择性抑制剂,能够作用于BMDMs(IC50:7.5 nM) 和 HMDMs(IC50:8.1 nM)。
T21509 CA 074

Cysteine Protease Proteases/Proteasome
CA 074 是一种高效的组织蛋白酶B (cathepsin B) 抑制剂, Ki 值为2 to 5 nM。CA 074 抑制灵长类动物缺血性海马神经元死亡,可减轻 SJL/J 小鼠诱导的实验性自身免疫性脑脊髓炎的视网膜病变和视神经炎。
T22398 Phenidone

菲尼酮,1-phenyl-3-pyrazolidinone

Lipoxygenase; COX Immunology/Inflammation; Metabolism; Neuroscience
Phenidone (1-phenyl-3-pyrazolidinone) 是可口服发环氧化酶和脂氧合酶双重抑制剂,可改善实验性自身免疫性脑脊髓炎大鼠的瘫痪,降低自发性高血压大鼠的血压,可用作照片显像剂。
T0511 Tolperisone hydrochloride

盐酸托哌酮,Muscalm,Midocalm,托哌酮盐酸盐,Tolperisone HCl

Sodium Channel Membrane transporter/Ion channel
Tolperisone hydrochloride (Muscalm) 是中枢作用肌肉松弛剂,可用于研究神经疾病引起的病理性横纹肌硬化(锥体束损伤、脊髓病、多发性硬化症、脑脊髓炎)、痉挛性麻痹及其他肌肉张力障碍相关的脑病。
T30529 BMS-520

BMS-520 is a potent, selective S1P1 agonist that has shown impressive efficacy when administered orally in a rat model of arthritis and in a mouse model of experimental autoimmune encephalomyelitis (EAE) with multiple sclerosis.
T82424 Experimental allergic encephalitogenic peptide (human)

Experimental allergic encephalitogenic peptide (human) 为EAE多肽类化合物,能够诱导豚鼠发生脑脊髓炎。
T81734 Myelin Basic Protein (1-11)

Myelin Basic Protein (1-11) 是髓鞘碱性蛋白 (MBP) 的一个致脑炎表位,并且常用于诱导实验性自身免疫性脑脊髓炎 (EAE)。
TP2080 ADWX 1

Potent and selective KV1.3 channel blocker (IC50 values are 0.0019 and 0.65 nM for KV1.3 and KV1.1, respectively). Inhibits CD4+ CCR7- T cell activation. Ameliorates rat experimental autoimmune encephalomyelitis, in a model for multiple sclerosis.
T69066 Forphenicine

Forphenicine is a bacterial metabolite that has been found in S. fulvoviridis and an inhibitor of alkaline phosphatase (IC50 = 0.036 µg/ml for the chicken intestine enzyme). It inhibits the growth of HL-60 leukemia cells when used at a concentration of 10 µM. Forphenicine (50 and 500 µg/animal) increases survival in a guinea pig model of experimental autoimmune encephalomyelitis (EAE).
T36766 Palmitoylcholine (chloride)

Palmitoylcholine is an acyl choline.1It inhibits protein kinase C activity when used at a concentration of 100 μM.2Palmitoylcholine induces hemolysis in rat erythrocytes.3Plasma levels of palmitoylcholine are decreased in female patients with myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS).1 1.Germain, A., Barupal, D.K., Levine, S.M., et al.Comprehensive circulatory metabolomics in ME/CFS reveals disrupted metabolism of acyl lipids and steroidsMetabolites10(1)34(2020) 2.Nakadate, T.,...
T63206 SR12418

SR12418 是一种特异性的 REV-ERB 合成配体,能够作用于 REV-ERBα (IC50: 68 nM) 和 REV-ERBβ (IC50: 119 nM),可用于研究实验性自身免疫性脑脊髓炎 (EAE) 和结肠炎。
T78031 MOG peptide (35-55)

MOG peptide (35-55) 是一段特定的髓鞘少突胶质细胞糖蛋白 (MOG) 免疫原肽的35至55氨基酸序列。该肽段具有针对CD4+T细胞的特异性活性,并可用于诱导实验性自身免疫性脑脊髓炎 (EAE) 的动物模型。
T82621 D359-0396

NOD-like Receptor (NLR) Immunology/Inflammation
D359-0396 是一种口服活性的 NLRP3 炎性体抑制剂,能有效抑制巨噬细胞焦亡(pyroptosis)以及 IL-1β 的释放,并阻止 NLRP3 和 ASC 的寡聚化,抑制 GSDMD 的裂解。该化合物在动物模型中能减轻小鼠的 EAE 症状,并提高感染性休克后的小鼠存活率。
T82020 J5 peptide

Myelin basic protein (85-99) antagonist

J5 peptide是MBP抑制剂,竞争性阻断MBP85-99与HLA-DR2的结合。该肽段能减轻PLP139-151/MBP85-99诱导的小鼠实验性自身免疫性脑脊髓炎(EAE)。J5 peptide主要用于研究炎症和免疫疾病。
T39110 MOG (35-55), human

MOG (35-55), human, a constituent of central nervous system myelin, is distinguishable from mMOG (35-55) due to a proline-to-serine substitution at position 42. It possesses immunogenic properties and is partially cross-reactive with mMOG35–55. However, MOG (35-55), human does not induce encephalitogenic effects, and only elicits minimal clinical signs of EAE (experimental autoimmune encephalomyelitis) in comparison to the rodent peptide.
T63141 ASP-4058 hydrochloride

ASP-4058 hydrochloride 是一种选择性的、口服具有活力的的鞘氨醇磷酸受体 1 和 5 (S1P1and S1P5) 的二代激动剂。ASP-4058 hydrochloride 安全性良好,能够改善小鼠实验性自身免疫性脑脊髓炎。
T72017 6(5H)-Phenanthridinone

6(5H)-Phenanthridinone is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2. It decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells. 6(5H)-Phenanthridinone reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes. In vivo, 6(5H)-phenanthridinone reduces spinal cord expression of inducible nitric oxide synthase (iNOS), IL-1β, TNF-α, IL-2, and IFN-γ and reduces disease score in a rat model of experimenta...
T73336 Ketotifen

酮替芬,HC 20-511

Ketotifen (HC 20-511)为第二代口服活性非竞争性组胺1(H1)受体阻滞剂兼肥大细胞稳定剂,能体外阻断6-磷酸葡萄糖酸脱氢酶(6-PGD)。其对SARS-CoV-2及流感病毒(Influenza virus)展现出抗病毒活性,适用于自身免疫性脑脊髓炎(EAE)与哮喘发作预防研究。
T36015 PDMP (hydrochloride)

PDMP is a ceramide analog first prepared in a search for inhibitors of glucosylceramide synthase. PDMP has two adjacent chiral centers (C1 and C2) allowing for the formation of four possible isomers. PDMP contains all four of these stereoisomers. PDMP inhibits glucosylceramide synthase by 90% when used at a concentration of 0.8 μM in MDCK cell homogenates, however, the ability to inhibit glucosylceramide synthase has been found to reside in the D-threo (1R,2R) enantiomer. The D-threo PDMP enanti...
T80682 γ-Fibrinogen 377-395 TFA

γ-Fibrinogen377-395 TFA 是纤维蛋白原衍生抑制肽,具有纤维蛋白原表位特性。该化合物能在体外抑制小胶质细胞激活、阻断纤维蛋白与Mac-1相互作用,并在小鼠体内抑制实验性自身免疫性脑脊髓炎(EAE)。该肽适用于多发性硬化症(MS)及其他血脑屏障损伤和小胶质细胞激活相关的神经炎症疾病研究。
T80683 γ-Fibrinogen 377-395

γ-Fibrinogen377-395是一种衍自纤维蛋白原的抑制性肽段,也被认为是纤维蛋白原的表位之一。它能在体外抑制小胶质细胞的激活并阻断纤维蛋白与Mac-1的交互作用;此外,在小鼠体内能够抑制实验性自身免疫性脑脊髓炎(EAE)的发展。因此,γ-Fibrinogen377-395对于多发性硬化症(MS)以及其他与血脑屏障损伤和小胶质细胞活化相关的神经炎症性疾病的研究具有潜在的应用价值。
T81772 MOG (92–106), mouse, rat

MOG (92–106), mouse, rat 是一种来自小鼠/大鼠髓磷脂少突胶质细胞糖蛋白的生物活性肽,包含氨基酸片段92至106。在MOG (92–106) 诱导的实验性自身免疫性脑脊髓炎模型中,小鼠会对次级髓磷脂抗原呈现出广泛的B细胞反应性,尽管T细胞反应较弱。该肽段在SJL小鼠、DA大鼠以及恒河猴中均可诱导严重的脑炎。
T69600 Spermidine-d6

Spermidine-d6 is intended for use as an internal standard for the quantification of spermidine by GC- or LC-MS. Spermidine is an endogenous polyamine. It is formed from putrescine by spermidine synthase. Spermidine (25 µM) inhibits the activity of the human inward-rectifying potassium channel Kir2.3 in a patch-clamp assay. It induces autophagy in HeLa cells when used at a concentration of 100 µM and increases the lifespan of D. melanogaster, yeast, and C. elegans. Spermidine (30 mM in the drinki...
T36296 BIO5192 hydrate

BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2]. The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1].BIO5192 hydrate (30 mg/kg; s.c; bid; during days...
T83690 [Leu144, Arg147]-PLP (139-151) TFA

[Leu144, Arg147] Proteolipid Peptide (139-151),H-His-Ser-Leu-Gly-Lys-Leu-Leu-Gly-Arg-Pro-Asp-Lys-Phe-OH

[Leu144,Arg147]-PLP (139-151)是髓鞘脂蛋白(PLP)的一种突变肽段,包含位于144和147位置的色氨酸到亮氨酸以及组氨酸到精氨酸的替换。使用[Leu144, Arg147]-PLP (139-151)(50 µg)乳化于完全弗氏佐剂(CFA)免疫后,能增加小鼠脾脏中的IL-4水平。它在体外抑制Th1细胞激活,但在体内不抑制,其中它诱导调节性T细胞的产生。用[Leu144, Arg147]-PLP (139-151)预免疫可以延迟由脑炎肽PLP (178-191)、髓磷脂少突细胞蛋白(MOG) (92-106)或髓鞘基础蛋白(MBP)在小鼠中诱导的实验性自身免疫性脑炎(EAE)的发病。
T83688 R 715 TFA

[Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH

R 715是一种布拉迪肾上腺素B1受体拮抗剂。它抑制在表达布拉迪肾上腺素B1受体的孤立人类脐带中由布拉迪肾上腺素引发的收缩(pA2 = 8.49)。R 715(200、400及600 µg/kg)通过尾部闪烁测试减少了由链脲佐菌素(STZ)诱导的糖尿病神经病变小鼠模型中尾部撤回的潜伏期。它还在以髓磷脂少突胶质细胞糖蛋白(MOG)(35-55)(MOG35-55)抗原肽诱导的实验性自体免疫性脑炎(EAE)小鼠模型中,通过每天1 mg/kg的剂量减少了后肢无力和瘫痪的发病率,改善对称步态,并减少脊髓炎症灶点数、神经元脱髓鞘以及病灶单核细胞侵袭。R 715(0.01 nmol/动物,脑室内)能在自发性高血压大鼠中降低平均动脉血压并增加心率。
T83910 S1PL-IN-31

Sphingosine-1-Phosphate Lyase Inhibitor 31,S1PL Inhibitor 31,S1P Lyase Inhibitor 31

S1PL-IN-31是一种鞘氨醇-1-磷酸(S1P)裂解酶的抑制剂(IC50 = 210 nM),同时也是Smoothened(Smo)受体的对抗剂(IC50 = 440 nM)。在体内,S1PL-IN-31 (每天2 mg/kg)能够防止实验性自身免疫性脑炎(EAE)模型大鼠中,由髓鞘少突胶质细胞糖蛋白(MOG)肽段MOG29-152诱发的颈部及胸部淋巴细胞渗透和神经肌肉虚弱。该化合物降低了大鼠的淋巴细胞总数及CD4+ T细胞、CD8+ T细胞和B细胞的水平。S1PL-IN-31 (每天3及10 mg/kg剂量)在雄性和雌性大鼠心脏和淋巴结中增加了S1P水平,并且在雌性大鼠中降低了心率。
T38106 JC-171

JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages[1]. JC-171 (0-100 μM) blocks NLRP3 inflammasome activation and IL-1β production in primary macrophages dose dependently[1]. ...

化合物

glatiramer Acetate
Cat.No: TP2315
Synonym:
Target: Others
NIBR-0213
Cat.No: T28169
Synonym: NIBR 0213
Target: LPL Receptor
5J-4
Cat.No: T24984
Synonym:
Target: Calcium Channel
Luzindole
Cat.No: T15795
Synonym: N-乙酰-2-苄基色胺,N-0774
Target: Melatonin Receptor, MT Receptor
Ketotifen fumarate
Cat.No: T0994
Synonym: HC 20511 fumarate,富马酸酮替芬
Target: PDE, Histamine Receptor
Cenerimod
Cat.No: T14924
Synonym: ACT-334441
Target: S1P Receptor
Lenaldekar
Cat.No: T24398
Synonym: LDK
Target: Akt, IGF-1R, S6 Kinase
24, 25-Dihydroxy VD2
Cat.No: T19107
Synonym: 24,25-Dihydroxy vitamin D2
Target: Vitamin
PF-04957325
Cat.No: T12422
Synonym:
Target: PDE
3-Methoxycatechol
Cat.No: T77555
Synonym: 1,2-Dihydroxy-3-methoxybenzene
Target: Antiviral
ASP-4058
Cat.No: T10385
Synonym:
Target: S1P Receptor, LPL Receptor
MCC950
Cat.No: T3701
Synonym: CP-456773
Target: NOD
CA 074
Cat.No: T21509
Synonym:
Target: Cysteine Protease
Phenidone
Cat.No: T22398
Synonym: 菲尼酮,1-phenyl-3-pyrazolidinone
Target: Lipoxygenase, COX
Tolperisone hydrochloride
Cat.No: T0511
Synonym: 盐酸托哌酮,Muscalm,Midocalm,托哌酮盐酸盐,Tolperisone HCl
Target: Sodium Channel
BMS-520
Cat.No: T30529
Synonym:
Target:
Experimental allergic encephalitogenic peptide (human)
Cat.No: T82424
Synonym:
Target:
Myelin Basic Protein (1-11)
Cat.No: T81734
Synonym:
Target:
ADWX 1
Cat.No: TP2080
Synonym:
Target:
Forphenicine
Cat.No: T69066
Synonym:
Target:
Palmitoylcholine (chloride)
Cat.No: T36766
Synonym:
Target:
SR12418
Cat.No: T63206
Synonym:
Target:
MOG peptide (35-55)
Cat.No: T78031
Synonym:
Target:
D359-0396
Cat.No: T82621
Synonym:
Target: NOD-like Receptor (NLR)
J5 peptide
Cat.No: T82020
Synonym: Myelin basic protein (85-99) antagonist
Target:
MOG (35-55), human
Cat.No: T39110
Synonym:
Target:
ASP-4058 hydrochloride
Cat.No: T63141
Synonym:
Target:
6(5H)-Phenanthridinone
Cat.No: T72017
Synonym:
Target:
Ketotifen
Cat.No: T73336
Synonym: 酮替芬,HC 20-511
Target:
PDMP (hydrochloride)
Cat.No: T36015
Synonym:
Target:
γ-Fibrinogen 377-395 TFA
Cat.No: T80682
Synonym:
Target:
γ-Fibrinogen 377-395
Cat.No: T80683
Synonym:
Target:
MOG (92–106), mouse, rat
Cat.No: T81772
Synonym:
Target:
Spermidine-d6
Cat.No: T69600
Synonym:
Target:
BIO5192 hydrate
Cat.No: T36296
Synonym:
Target:
[Leu144, Arg147]-PLP (139-151) TFA
Cat.No: T83690
Synonym: [Leu144, Arg147] Proteolipid Peptide (139-151),H-His-Ser-Leu-Gly-Lys-Leu-Leu-Gly-Arg-Pro-Asp-Lys-Phe-OH
Target:
R 715 TFA
Cat.No: T83688
Synonym: [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH
Target:
S1PL-IN-31
Cat.No: T83910
Synonym: Sphingosine-1-Phosphate Lyase Inhibitor 31,S1PL Inhibitor 31,S1P Lyase Inhibitor 31
Target:
JC-171
Cat.No: T38106
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T3426 Bacoside A

MMP; Others; TNF; Dopamine Receptor; NOS; ROS Apoptosis; GPCR/G Protein; Immunology/Inflammation; Neuroscience; Others; Proteases/Proteasome
Bacoside A has a possible anticancer activity that could be inducing cell cycle arrest and apoptosis through Notch pathway in GBM in vitro. It exerts cytoprotective efficacy by attenuation of ROS generated through oxidative stress by an increase in the concentration of antioxidant enzymes and sustain membrane integrity which leads to restoring the damage caused by tBHP. Bacoside A can able to inhibit the progression of Experimental Autoimmune Encephalomyelitis (EAE) may be by the inhibition of i...
T36845 Isogarcinol

Isogarcinol is a natural polyisoprenylated benzophenone first isolated from plant species in the genus Garcinia. It has immunosuppressant actions, inhibiting the protein phosphatase calcineurin (IC50 = 36 μM) and suppressing the proliferation of T cells. Oral administration of isogarcinol in mice decreases delayed type hypersensitivity, prolongs graft survival in allogeneic skin transplants, suppresses inflammation in collagen-induced arthritis, and reduces clinical symptoms in experimental auto...
T78492 D-Mannuronic acid sodium

D-Mannuronic acid sodium,一种可从Macrocystis pyrifera中分离得到的化合物,显示出在自身免疫性脑脊髓炎(EAE)、佐剂性关节炎(AIA)、肾病综合征以及急性肾小球肾炎的研究中具有潜在应用价值。

天然产物

Bacoside A
Cat.No: T3426
Synonym:
Target: MMP, Others, TNF, Dopamine Receptor, NOS, ROS
Isogarcinol
Cat.No: T36845
Synonym:
Target:
D-Mannuronic acid sodium
Cat.No: T78492
Synonym:
Target:
TargetMol Loading
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